Abstract

Purpose: To evaluate the in vitro anti-oxidant and anti-inflammatory potential of the most potent and abundant metabolite, 3-methoxy quercetin (3-MQ), from extract fractions of mistletoe, Loranthus micranthus Linn (Loranthaceae) parasitic on Kola acuminata Schott & Endl, (Malvaceae), also known as Garcinia kola Heckel, (Clusiaceae). Methods: Compounds isolated through a combination of chromatographic techniques were screened for in vitro antioxidant potential using the diphenyl picrazyl hydrazine (DPPH) radical-based model. Cell viability at 1–1000 μM 3-MQ in 24 h was evaluated by 3-(4, 5-dimethylthiazol-2-yl)-2, 5- diphenyltetrazolium bromide (MTT) test. Lipopolysaccharide (LPS), phorbol 12-myristate 13-acetate (n = 5) five (5) replicates. Results: Ten (10) known compounds including 3-MQ (1) were isolated and characterized. 3-MQ exhibited highly significant (p < 0.05) antioxidant activity with 50 % inhibitory concentration (IC 50 ) of 15.0 μM; concentrations ≤ 100 μM did not exert cytotoxic effect. 3-MQ, at 25 and 125 μM concentrations, significantly (p < 0.05) inhibited the production of TNF-α by 82 and 100 %, respectively, compared to controls. Conclusion: The results demonstrate the potent anti-inflammatory activity of 3-MQ and suggests its use as a potential alternative therapy for inflammation and related diseases. Keywords: Loranthus micranthus , Kola acuminata , Garcinia kola , Anti-inflammatory, Cytotoxicity, Chemiluminescence, Antioxidant, TNF-α

Highlights

  • Plant-derived natural products, including the quercetin-derivatives, are ubiquitous and undoubtedly form interesting scaffolds for the development of potent antioxidant-antiinflammatory as well as possible antitumor congeners

  • Out of the ten compounds tested (Figure 1), compound 1 (3-MQ) exhibited highly significant (p

  • Regarding the anti-inflammatory property, ROS and RNS release by activated RAW264.7 cells was significantly inhibited by 3-methoxy quercetin (3-MQ).p

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Summary

INTRODUCTION

Plant-derived natural products, including the quercetin-derivatives, are ubiquitous and undoubtedly form interesting scaffolds for the development of potent antioxidant-antiinflammatory as well as possible antitumor congeners This is illustrated by the fact that in the flavonol group alone, over 230 new compounds were identified from 1986 to 1992 [1], while approximately 180 new structures were isolated in the subsequent years 2001-2003 [2]. The sub-fractions with substantial yields were either subjected to semipreparative HPLC or sephadex column to obtain pure compounds 3-9. This was repeated for the n-butanol fraction (22.7 g) to obtain compounds 2 and 10. Student’s ‘t’ test was used to study statistical significance (p

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Conflict of Interest

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